Tranylcypromine

Tranylcypromine Uses, Dosage, Side Effects, Food Interaction and all others data.

A propylamine formed from the cyclization of the side chain of amphetamine. This monoamine oxidase inhibitor is effective in the treatment of major depression, dysthymic disorder, and atypical depression. It also is useful in panic and phobic disorders (From AMA Drug Evaluations Annual, 1994, p311).

Tranylcypromine is a racemate comprising equal amounts of (1R,2S)- and (1S,2R)-2-phenylcyclopropan-1-amine with the chiral centers both located on the cylopropane ring. An irreversible monoamine oxidase inhibitor that is used as an antidepressant (INN tranylcypromine).

Tranylcypromine belongs to a class of antidepressants called monoamine oxidase inhibitors (MAOIs). Tranylcypromine is a non-hydrazine monoamine oxidase inhibitor with a rapid onset of activity. MAO is an enzyme that catalyzes the oxidative deamination of a number of amines, including serotonin, norepinephrine, epinephrine, and dopamine. Two isoforms of MAO, A and B, are found in the body. MAO-A is mainly found within cells located in the periphery and catalyzes the breakdown of serotonin, norepinephrine, epinephrine, dopamine and tyramine. MAO-B acts on phenylethylamine, norepinephrine, epinephrine, dopamine and tyramine, is localized extracellularly and is found predominantly in the brain. While the mechanism of MAOIs is still unclear, it is thought that they act by increasing free serotonin and norepinephrine concentrations and/or by altering the concentrations of other amines in the CNS. It has been postulated that depression is caused by low levels of serotonin and/or norepinephrine and that increasing serotonergic and norepinephrinergic neurotransmission results in relief of depressive symptoms. MAO A inhibition is thought to be more relevant to antidepressant activity than MAO B inhibition. Selective MAO B inhibitors, such as selegiline, have no antidepressant effects.

Tranylcypromine
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Tranylcypromine
Availability	Prescription only
Generic	Tranylcypromine
Tranylcypromine Other Names	dl-tranylcypromine, Racemic Tranylcypromine, Tranilcipromina, Transamine, Tranylcypromin, Tranylcypromine, Tranylcyprominum
Related Drugs	Rexulti, sertraline, trazodone, Lexapro, Zoloft, citalopram, Cymbalta
Weight	10mg
Type	Tablet, Oral Tablet
Formula	C₉H₁₁N
Weight	Average: 133.194 Monoisotopic: 133.089149358
Groups	Approved, Investigational
Therapeutic Class
Manufacturer	ADVANZ Pharma
Available Country	United Kingdom, United States
Last Updated:	September 19, 2023 at 7:00 am

Uses

Tranylcypromine is a monoamine oxidase inhibitor used to treat major depressive disorder.

For the treatment of major depressive episode without melancholia.

Tranylcypromine is also used to associated treatment for these conditions: Acute Depressive Episode

How Tranylcypromine works

Tranylcypromine irreversibly and nonselectively inhibits monoamine oxidase (MAO). Within neurons, MAO appears to regulate the levels of monoamines released upon synaptic firing. Since depression is associated with low levels of monoamines, the inhibition of MAO serves to ease depressive symptoms, as this results in an increase in the concentrations of these amines within the CNS.

Toxicity

In overdosage, some patients exhibit insomnia, restlessness and anxiety, progressing in severe cases to agitation, mental confusion and incoherence. Hypotension, dizziness, weakness and drowsiness may occur, progressing in severe cases to extreme dizziness and shock. A few patients have displayed hypertension with severe headache and other symptoms. Rare instances have been reported in which hypertension was accompanied by twitching or myoclonic fibrillation of skeletal muscles with hyperpyrexia, sometimes progressing to generalized rigidity and coma.

Food Interaction

Avoid alcohol. Ingesting alcohol may increase the CNS depressant effects of tranylcypromine.
Avoid St. John's Wort. Administering tranylcypromine with St. John's Wort may increase the risk of serotonin syndrome.
Avoid tyramine-containing foods and supplements. Tyramine-containing foods and beverages can cause a sudden elevation in blood pressure or a hypertensive crisis. Foods that contain tyramine include aged cheese, ripe bananas, red wine, some alcoholic beverages (beer), cured food, pickled food, and fava beans.

[Major] CONTRAINDICATED: Foods that contain large amounts of tyramine may precipitate a hypertensive crisis in patients treated with monoamine oxidase inhibitors (MAOIs).

The mechanism is inhibition of MAO-A, the enzyme responsible for metabolizing exogenous amines such as tyramine in the gut and preventing them from being absorbed intact.

Once absorbed, tyramine is metabolized to octopamine, a substance that is believed to displace norepinephrine from storage granules.

GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of MAOIs.

Use in combination may result in additive central nervous system depression and
MANAGEMENT: In general, patients treated with MAOIs or other agents that possess MAOI activity (e.g., furazolidone, linezolid, procarbazine) should avoid consumption of products that contain large amounts of amines and protein foods in which aging or breakdown of protein is used to increase flavor.

These foods include cheese (particularly strong, aged or processed cheeses), sour cream, wine (particularly red wine), champagne, beer, pickled herring, anchovies, caviar, shrimp paste, liver (particularly chicken liver), dry sausage, salamis, figs, raisins, bananas, avocados, chocolate, soy sauce, bean curd, sauerkraut, yogurt, papaya products, meat tenderizers, fava bean pods, protein extracts, yeast extracts, and dietary supplements.

Caffeine may also precipitate hypertensive crisis so its intake should be minimized as well.

At least 14 days should elapse following discontinuation of MAOI therapy before these foods may be consumed.

Specially designed reference materials and dietary consultation are recommended so that an appropriate and safe diet can be planned.

Patients should be advised to promptly seek medical attention if they experience potential signs and symptoms of a hypertensive crisis such as severe headache, visual disturbances, difficulty thinking, stupor or coma, seizures, chest pain, unexplained nausea or vomiting, and stroke-like symptoms.

Patients should also be counseled not to use MAOIs with alcohol, and to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them.

Tranylcypromine Drug Interaction

Major: citalopram, selegiline, escitalopram, vortioxetineModerate: aripiprazole, suvorexant, diphenhydramine, clonazepam, lurasidone, lithium, pregabalin, metoprolol, metoprolol, quetiapineUnknown: levothyroxine, mometasone nasal, acetaminophen, levothyroxine, cyanocobalamin, cholecalciferol

Tranylcypromine Disease Interaction

Major: blood pressure, carcinoid syndrome, headaches, hyperthyroidism, liver disease, pheochromocytoma, renal dysfunction, alcohol, depression, hypertension/CVD, liver disease, pheochromocytomaModerate: hypoglycemia, parkinsonism, schizophrenia/bipolar, seizures, angina, bipolar disorder screening, diabetes, hypotension, renal disease, seizures

Volume of Distribution

1.1-5.7 L/kg

Elimination Route

Interindividual variability in absorption. May be biphasic in some individuals. Peak plasma concentrations occur in one hour following oral administration with a secondary peak occurring within 2-3 hours. Biphasic absorption may represent different rates of absorption of the stereoisomers of the drug, though additional studies are required to confirm this.